dBET1 _PROTAC - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEdBET1Cat. No.: HY-101838CAS No.: 1799711-21-9分式: CHClNOS分量: 785.27作靶点: Epigenetic Reader Domain; PROTAC作通路: Epigenetics; PROTAC储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 50 mg/mL (63.6

2、7 mM)H2O : 90% corn oilSolubility: 3 mg/mL (3.82 mM); Clear solutionBIOLOGICAL ACTIVITY1/2 Master of Small Molecules 您边的抑制剂师www.MedChemE物活性 dBET1于 PROTAC 技术的有效的 BRD4 蛋质降解物，其 EC50 值为 430 nM。IC50 & Target EC50: 430 nM (BRD4) 1体外研究 Treatment with dBET1 down regulates MYC and PIM1 transcription. Degrada

3、tion of BRD4 by dBET1 isassociated with a more potent apoptotic consequence in MV4;11 cell line. Significantly increased apoptosisafter only 4 h of dBET1 treatment is enhanced at 8 h. dBET1 also induces a potent and superior inhibitoryeffect on MV4;11 cell proliferation at 24 hours (measured by ATP

4、content, IC50= 0.14 M, compare to IC50=1.1 M with JQ1) 1.体内研究 Administration of dBET1 attenuates tumor progression as determined by serial volumetric measurement, anddecreases tumor weight assessed post-mortem. Acute pharmacodynamic degradation of BRD4 is observedfour hours after a first or second d

5、aily treatment with dBET1 (50 mg/kg IP). A statistically significantdestabilization of BRD4, down regulation of MYC and inhibition of proliferation is observed with dBET1compare to vehicle control in excised tumors. Two weeks of dBET1 is well tolerated by mice without ameaningful effect on weight, w

6、hite blood count, hematocrit or platelet count 1.REFERENCES1. Winter GE, et al. DRUG DEVELOPMENT. Phthalimide conjugation as a strategy for in vivo target protein degradation. Science. 2015Jun 19;348(6241):1376-81.McePdfHeightCaution: Product has not been fully validated for medical applications.For research use only.Tel: 400-82